440841

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关键词:'440841'

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Didier, E. et al.

Tetrahedron, 47, 4941-4941 (1991)

Inhibitors of the protease from human immunodeficiency virus: synthesis, enzyme inhibition, and antiviral activity of a series of compounds containing the dihydroxyethylene transition-state isostere.

S Thaisrivongs et al.

Journal of medicinal chemistry, 36(8), 941-952 (1993-04-16)

A number of potential HIV protease inhibitory peptides that contain the dihydroxyethylene isostere were prepared and evaluated for their enzyme binding affinity and antiviral activity in cell cultures. From the template of a previously reported active peptide A, modifications at

Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.

W J Thompson et al.

Journal of medicinal chemistry, 35(10), 1685-1701 (1992-05-15)

By tethering of a polar hydrophilic group to the P1 or P1' substituent of a Phe-based hydroxyethylene isostere, the antiviral potency of a series of HIV protease inhibitors was improved. The optimum enhancement of anti-HIV activity was observed with the

Thompson, W.J. et al.

Tetrahedron Letters, 33, 2957-2957 (1992)

B. Di Simone et al.

Tetrahedron Asymmetry, 6, 301-301 (1995)

HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.

S D Young et al.

Journal of medicinal chemistry, 35(10), 1702-1709 (1992-05-15)

A systematic investigation was undertaken to determine the role of the P1' sidechain in a series of hydroxyethylene isostere based inhibitors of HIV-1 protease. Substitution and homologation of the benzyl P1' side chain of the Phe-Phe isostere based pseudo peptides

D'Aniello, F. et al.

The Journal of Organic Chemistry, 59, 3762-3762 (1994)

Askin, D. et al.

The Journal of Organic Chemistry, 57, 2771-2771 (1992)

Dorsey, B.D. et al.

Tetrahedron Letters, 34, 1851-1851 (1993)

A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity.

T J Tucker et al.

Journal of medicinal chemistry, 35(14), 2525-2533 (1992-07-20)

A series of HIV-1 protease inhibitors containing a novel hydroxyethyl secondary amine transition state isostere has been synthesized. The compounds exhibit a strong preference for the (R) stereochemistry at the transition state hydroxyl group. Molecular modeling studies with the prototype

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